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Published on: June 10, 2021
Difluorocarbene-Enabled [2+1+3] Cyclization for the Synthesis of Pyrimidin-4-ones
Chun-Yan Wu1, Yu-Jia Fan1, Li-Sheng Wang1
1State Key Laboratory of Green Pesticide, International Joint Research Center for Intelligent Biosensor Technology and Health, College of Chemistry, Central China Normal University, Wuhan, Hubei 430079, China.
None:
A difluorocarbene-mediated [2+1+3] cyclization carbonylation for the efficient construction of the pyrimidin-4-one skeleton has been reported. Using sulfoxonium ylides, BrCF2CO2Et, and amidines as starting materials, the method features operational simplicity and readily available substrates. Mechanistic studies confirmed the formation of difluorocarbene. This work expands the application of difluorocarbene as a carbonyl synthon and provides a new route for the synthesis of pyrimidinone derivatives.
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